{"product_id":"afatinib-dimaleate-bhb21900092","title":"Afatinib dimaleate","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}.bhp-desc p{margin:0 0 12px}.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}.bhp-desc .bhp-cat-pill{display:inline-block;background:#003366;color:#fff;border-radius:20px;padding:3px 12px;font-size:13px;margin-bottom:10px}\u003c\/style\u003e\n\u003cspan class=\"bhp-cat-pill\"\u003eInhibitors\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003eAfatinib dimaleate, also known as BIBW 2992MA2, is an orally active, potent, irreversible dual-specificity inhibitor of the ErbB family (EGFR and HER2), with IC\u003csub\u003e50\u003c\/sub\u003e values of 0.5 nM for EGFR wt, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R\/T790M, and 14 nM for HER2. It can be used to study esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer\u003csup\u003e[1][2][3][4]\u003c\/sup\u003e. It is supplied as a white to yellow solid (C32H33ClFN5O11, MW 718.08) at 99.74% purity.\u003c\/p\u003e\n\u003ch2\u003ePhysical \u0026amp; Chemical Properties\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\u003ctbody\u003e\n\u003ctr\u003e\n\u003cth\u003eCAS Number\u003c\/th\u003e\n\u003ctd\u003e850140-73-7\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC32H33ClFN5O11\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e718.08 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.74%\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eAppearance\u003c\/th\u003e\n\u003ctd\u003eSolid\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eColor\u003c\/th\u003e\n\u003ctd\u003eWhite to yellow\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eO=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CCOC4)\/C=C\/CN(C)C.O=C(O)\/C=C\\C(O)=O.O=C(O)\/C=C\\C(O)=O\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003eEGFR L858R, EGFR, EGFR L858R\/T790M, HER2, HER3\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eJAK\/STAT Signaling; Protein Tyrosine Kinase\/RTK; Autophagy; Apoptosis; PI3K\/Akt\/mTOR; MAPK\/ERK Pathway\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: 100 mg\/mL (139.26 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)\u003cbr\u003eH2O: 50 mg\/mL (69.63 mM; Requires sonication)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003e4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eRoom temperature in continental US; may vary elsewhere.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eBiological Activity\u003c\/h2\u003e\n\u003ch3 style=\"font-size:16px;font-weight:700;color:#003366;margin:16px 0 8px\"\u003eIC50 \u0026amp; Target\u003csup\u003e[1]\u003c\/sup\u003e\n\u003c\/h3\u003e\n\u003cp\u003e\u003c\/p\u003e\n\u003ctable\u003e\u003ctbody\u003e\u003ctr\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eEGFR\u003csup\u003eL858R\u003c\/sup\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.4 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eEGFR\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.5 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eEGFR\u003csup\u003eL858R\/T790M\u003c\/sup\u003e\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e10 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eHER2\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e14 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003c\/tr\u003e\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eLiterature Cited\u003c\/h2\u003e\n\u003cp style=\"font-size:14px;color:#555;margin:0 0 10px\"\u003e\u003cem\u003eSources cited in this description and in the In Vitro \u0026amp; In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.\u003c\/em\u003e\u003c\/p\u003e\n\u003cp\u003e [1]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"http:\/\/www.ncbi.nlm.nih.gov\/pubmed\/18408761\"\u003eLi D, et al. BIBW2992, an irreversible EGFR\/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"http:\/\/www.ncbi.nlm.nih.gov\/pubmed\/26885448\"\u003eWong CH, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [3]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/25436978\"\u003eWang XK, et al. Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. Oncotarget. 2014 Dec 15;5(23):11971-85.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [4]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/29465762\"\u003eYoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176.\u003c\/a\u003e\u003c\/p\u003e\n\u003ch2\u003eSafety\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\u003cp\u003e\u003cstrong\u003eFor Research Use Only.\u003c\/strong\u003e Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.\u003c\/p\u003e\u003c\/div\u003e\n\u003c\/div\u003e","brand":"MedChemExpress (MCE)","offers":[{"title":"5 mg","offer_id":67604848542061,"sku":"HY-10261A-5MG","price":46.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605016346989,"sku":"HY-10261A-10MG","price":72.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605016379757,"sku":"HY-10261A-25MG","price":120.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605016412525,"sku":"HY-10261A-50MG","price":159.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605016445293,"sku":"HY-10261A-100MG","price":198.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605016478061,"sku":"HY-10261A-200MG","price":252.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605016510829,"sku":"HY-10261A-500MG","price":414.0,"currency_code":"USD","in_stock":true},{"title":"1 g","offer_id":67605016543597,"sku":"HY-10261A-1G","price":594.0,"currency_code":"USD","in_stock":true},{"title":"5 g","offer_id":67605016576365,"sku":"HY-10261A-5G","price":0.0,"currency_code":"USD","in_stock":true},{"title":"10 g","offer_id":67605016609133,"sku":"HY-10261A-10G","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67605016641901,"sku":"HY-10261A-1MLX10MM","price":72.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-10261a.gif?v=1790972872","url":"https:\/\/www.ebiohippo.com\/products\/afatinib-dimaleate-bhb21900092","provider":"BioHippo","version":"1.0","type":"link"}